Formulations and methods for vaginal delivery of antiprogestins

Abstract

The subject matter of the present invention is pertinent to the field of vaginal delivery of pharmaceutically active agents. Embodiments of the instant invention disclose methods for treating a variety of progesterone related disorders by vaginal administration of a pullulan capsule comprising one or more antiprogestins.

What is claimed is: 
     
       1. A method for treating a progesterone-dependent condition in a human female comprising administering to the vaginal mucosa of the female a mucoadhesive capsule comprising:
 85 to 90 wt % pullulan; potassium chloride in an amount of 1.0% to 1.5% by weight; carrageenan in an amount of 0.1% to 0.4% by weight; one or more surfactants in an amount of 0.1 to 0.2% by weights; and water; and 
 a fill formulation comprising the antiprogestin CDB-4124, and excipients comprising 30% to 60% w/w fatty acid esters, 30% to 60% w/w PEG 1000 and 0.1 to 5% w/w lecithin; 
 wherein the progesterone-dependent condition is selected from the group consisting of endometriosis, adenomyosis, edometriomas of the ovary, dysmenorrhea, uterine fibroids, endometrial hyperproliferation, ovarian cancer, and cervical cancer. 
 
     
     
       2. The method of  claim 1 , wherein the antiprogestin CDB-4124 is administered daily at a dosage of 1 mg to 50 mg. 
     
     
       3. The method of  claim 2 , wherein the antiprogestin CDB-4124 is administered at a dosage of 12.5 mg or less. 
     
     
       4. The method of  claim 3 , wherein the capsule comprises pullulan in an amount of 86.3% by weight, potassium chloride in an amount of 1.32% by weight, carrageenan in an amount of 0.27% by weight, surfactants selected from sugar esters, sorbitan monolaurate and combinations thereof in an amount of 0.15% by weight and water. 
     
     
       5. The method of  claim 4 , wherein the fill formulation consists essentially of the antiprogestin CDB-4124 and PEG 1000, and optionally butylated hydroxytoluene. 
     
     
       6. The method of  claim 4 , wherein the capsule is administered once per day.